Application of arylhydrazide compound in treatment of acute myocardial ischemic coronary heart disease

A technology for acute myocardial ischemia and coronary heart disease, applied in the field of medicine, to prolong the hypoxia tolerance time and increase the serum NO content

Inactive Publication Date: 2017-02-15
段占娥
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, in the treatment of coronary heart disease, there is no literature report on the drug with N-(2-(1H-indol-3-yl)acetyl)phenylacetylhydrazide as the main active ingredient.

Method used

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  • Application of arylhydrazide compound in treatment of acute myocardial ischemic coronary heart disease
  • Application of arylhydrazide compound in treatment of acute myocardial ischemic coronary heart disease
  • Application of arylhydrazide compound in treatment of acute myocardial ischemic coronary heart disease

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0011] Example 1: Preparation of N-(2-(1H-indol-3-yl)acetyl)phenylacetylhydrazide

[0012] (1) Add 8.8g (50mmol) of indole acetic acid (50mmol), methanol (60mL), and concentrated sulfuric acid (3mL) to a 500ml round bottom flask, and react at 70°C for 1-3 hours. water (50mL), separate the organic phase, extract the aqueous phase with ethyl acetate (3×20mL), combine the organic phases, wash with saturated sodium bicarbonate solution and water successively, dry over anhydrous sodium sulfate, and concentrate under reduced pressure to obtain indole Crude methyl acetate.

[0013] (2) Add 9.46g (48mmol) of methyl indole acetate, ethylene glycol methyl ether (40mL), and 5mL of hydrazine hydrate into a 500ml round-bottomed flask, heat and reflux at 115°C for about 20 hours, thin-layer chromatography (TLC) After detecting the disappearance of the raw material point, stop the reaction, cool to room temperature, add water (50 mL), stand still to precipitate a white solid, obtain the cru...

Embodiment 2

[0016] Example 2: Experimental study on the influence of N-(2-(1H-indol-3-yl)acetyl)phenylacetylhydrazide on serum NO content in rats with acute myocardial ischemia

[0017] Thirty male healthy Wistar rats, weighing 220-250 g, were randomly divided into the following three groups: normal control group, model control group, and compound test group, with 10 rats in each group. Based on the rat body weight, rats in the compound test group were intravenously injected with N-(2-(1H-indol-3-yl)acetyl)phenylacetylhydrazide 20mg / kg, and the model control group and the normal control group were intravenously injected, etc. volume of saline. Each group was injected once a day between 9:00-10:00 am for 7 consecutive days. Ten minutes after the injection on the 5th, 6th, and 7th day, except the normal control group, the rats in the other two groups were intraperitoneally injected with isoproterenol 2 mg / kg to create a rat model of acute myocardial ischemia. 24 hours after the last injec...

Embodiment 3

[0022] Example 3: Experimental study on the influence of N-(2-(1H-indol-3-yl)acetyl)phenylacetylhydrazine on the hypoxia tolerance time of acute myocardial ischemia mice

[0023] 50 healthy Kunming mice, weighing 18-22 g, half male and half male, were randomly divided into the following three groups: normal control group, model control group, and compound test group, with 10 mice in each group. Based on the body weight of the mice, the mice in the compound test group were intravenously injected with N-(2-(1H-indol-3-yl)acetyl)phenylacetylhydrazide 32 mg / kg, and the model control group and the normal control group were injected intravenously, etc. volume of saline. Each group was injected once a day between 9:00-10:00 am for 8 consecutive days. Ten minutes after the injection on the eighth day, except for the normal control group, 2 mg / kg of isoproterenol was subcutaneously injected into mice in each group to create a mouse model of acute myocardial ischemia. After each group...

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Abstract

The invention belongs to the technical field of medicine, and discloses an application of an arylhydrazide compound in the treatment of acute myocardial ischemic coronary heart disease. The arylhydrazide compound is N-(2-(1H-indole-3-yl)acetyl)phenyl acetic hydrazide. The provided arylhydrazide compound can increase the content of NO in serum of patients of acute myocardial ischemic coronary heart disease, and prolongs the hypoxia tolerance time to prevent the acute myocardial ischemic coronary heart disease. A novel drug for treating the disease is provided.

Description

technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to the application of an aromatic hydrazide compound in the treatment of acute myocardial ischemic coronary heart disease. Background technique [0002] Coronary atherosclerotic heart disease is a heart disease caused by atherosclerotic lesions in the coronary arteries that cause stenosis or blockage of the vessel lumen, resulting in myocardial ischemia, hypoxia or necrosis. It is often called "coronary heart disease". There are many types of coronary heart disease, including acute myocardial ischemic coronary heart disease, the basic pathology of which is coronary artery insufficiency, myocardial acute, temporary ischemia and hypoxia. Studies in recent years have shown that NO has strong vasodilation, inhibition of vascular smooth muscle cell proliferation, anti-platelet aggregation, adhesion and release of active substances, and can prevent vasospasm and thrombosis. V...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/405A61P9/10
CPCA61K31/405
Inventor 段占娥张文学
Owner 段占娥
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